TWI823878B - 嘧啶基胺基-吡唑化合物之多晶型物及固體形式及製備方法 - Google Patents

嘧啶基胺基-吡唑化合物之多晶型物及固體形式及製備方法 Download PDF

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TWI823878B
TWI823878B TW107141257A TW107141257A TWI823878B TW I823878 B TWI823878 B TW I823878B TW 107141257 A TW107141257 A TW 107141257A TW 107141257 A TW107141257 A TW 107141257A TW I823878 B TWI823878 B TW I823878B
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Taiwan
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polymorph
crystalline
methyl
compound
degrees
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TW107141257A
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English (en)
Chinese (zh)
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TW201925190A (zh
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卓維斯 里馬庫克
安安勒 蘇哈克
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美商戴納立製藥公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
TW107141257A 2017-11-21 2018-11-20 嘧啶基胺基-吡唑化合物之多晶型物及固體形式及製備方法 TWI823878B (zh)

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US201762589276P 2017-11-21 2017-11-21
US62/589,276 2017-11-21

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TW201925190A TW201925190A (zh) 2019-07-01
TWI823878B true TWI823878B (zh) 2023-12-01

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TW107141257A TWI823878B (zh) 2017-11-21 2018-11-20 嘧啶基胺基-吡唑化合物之多晶型物及固體形式及製備方法

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US (3) US10370361B2 (de)
EP (1) EP3717473B1 (de)
JP (1) JP7303821B2 (de)
KR (1) KR20200089713A (de)
CN (1) CN111819174A (de)
AR (1) AR113893A1 (de)
AU (1) AU2018372180B2 (de)
BR (1) BR112020010215A2 (de)
CA (1) CA3083022A1 (de)
CL (1) CL2020001346A1 (de)
CO (1) CO2020006206A2 (de)
CR (1) CR20200216A (de)
EA (1) EA202091279A1 (de)
IL (1) IL274824A (de)
JO (1) JOP20200128A1 (de)
MA (1) MA51222A (de)
MX (1) MX2020005332A (de)
PE (1) PE20210157A1 (de)
SG (1) SG11202004733WA (de)
TW (1) TWI823878B (de)
UA (1) UA126414C2 (de)
WO (1) WO2019104086A1 (de)

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KR20200089713A (ko) 2017-11-21 2020-07-27 데날리 테라퓨틱스 인크. 피리미디닐아미노-피라졸 화합물의 다형체와 고체 형태, 그리고 생산 방법
MX2020006641A (es) 2017-12-20 2021-01-08 Denali Therapeutics Inc Proceso para la preparacion de compuestos de pirimidinil-4-aminopi razol.
WO2023174946A1 (en) 2022-03-15 2023-09-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Early and non-invasive method for assessing a subject's risk of having parkinson's disease

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8815882B2 (en) * 2010-11-10 2014-08-26 Genentech, Inc. Pyrazole aminopyrimidine derivatives as LRRK2 modulators

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EP2574168B9 (de) 2010-05-21 2016-10-05 Incyte Holdings Corporation Topische formulierung für einen jak-hemmer
CA2797947C (en) 2010-06-04 2019-07-09 Charles Baker-Glenn Aminopyrimidine derivatives as lrrk2 modulators
GB201015949D0 (en) 2010-09-22 2010-11-03 Medical Res Council Technology Compounds
US8791130B2 (en) 2011-11-29 2014-07-29 Genentech, Inc. Aminopyrimidine derivatives as LRRK2 modulators
CA2850594C (en) 2011-11-29 2020-03-10 F. Hoffmann-La Roche Ag Aminopyrimidine derivatives as lrrk2 modulators
AR089182A1 (es) 2011-11-29 2014-08-06 Hoffmann La Roche Derivados de aminopirimidina como moduladores de lrrk2
ES2638595T3 (es) 2011-11-29 2017-10-23 Genentech, Inc. Derivados de aminopirimidina como moduladores de LRRK2
CN106279202A (zh) 2012-05-03 2017-01-04 霍夫曼-拉罗奇有限公司 作为lrrk2调节剂用于治疗帕金森病的吡唑氨基嘧啶衍生物
EP2844652B1 (de) 2012-05-03 2019-03-13 Genentech, Inc. Pyrazolaminopyrimidinderivate als lrrk2-modulatoren
CR20220182A (es) 2016-06-16 2022-06-15 Denali Therapeutics Inc Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos (divisional 2018-592)
KR20200089713A (ko) * 2017-11-21 2020-07-27 데날리 테라퓨틱스 인크. 피리미디닐아미노-피라졸 화합물의 다형체와 고체 형태, 그리고 생산 방법

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8815882B2 (en) * 2010-11-10 2014-08-26 Genentech, Inc. Pyrazole aminopyrimidine derivatives as LRRK2 modulators

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
期刊 Anthony A. Estrada etc. Discovery of Highly Potent, Selective, and Brain-Penetrant Aminopyrazole Leucine-Rich Repeat Kinase 2 (LRRK2) Small Molecule Inhibitors J. Med. Chem 2014, 57, 921−936， ACS publications 2014年01月15日 921−936，
期刊 Anthony A. Estrada etc. Discovery of Highly Potent, Selective, and Brain-Penetrant Aminopyrazole Leucine-Rich Repeat Kinase 2 (LRRK2) Small Molecule Inhibitors J. Med. Chem 2014, 57, 921-936， ACS publications 2014年01月15日 921-936， *

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Publication number Publication date
KR20200089713A (ko) 2020-07-27
EP3717473A4 (de) 2021-07-07
JOP20200128A1 (ar) 2020-05-21
CN111819174A (zh) 2020-10-23
SG11202004733WA (en) 2020-06-29
WO2019104086A1 (en) 2019-05-31
AU2018372180B2 (en) 2023-08-17
JP2021504450A (ja) 2021-02-15
PE20210157A1 (es) 2021-01-26
US20210087176A1 (en) 2021-03-25
TW201925190A (zh) 2019-07-01
EA202091279A1 (ru) 2020-08-19
US10851088B2 (en) 2020-12-01
UA126414C2 (uk) 2022-09-28
CL2020001346A1 (es) 2020-11-20
US20190315723A1 (en) 2019-10-17
MX2020005332A (es) 2021-01-08
CA3083022A1 (en) 2019-05-31
EP3717473B1 (de) 2024-01-10
CR20200216A (es) 2021-03-19
JP7303821B2 (ja) 2023-07-05
CO2020006206A2 (es) 2020-08-10
IL274824A (en) 2020-07-30
AR113893A1 (es) 2020-06-24
BR112020010215A2 (pt) 2020-11-03
US20190194170A1 (en) 2019-06-27
AU2018372180A1 (en) 2020-06-18
US11427571B2 (en) 2022-08-30
EP3717473A1 (de) 2020-10-07
US10370361B2 (en) 2019-08-06
MA51222A (fr) 2020-10-07

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